[D-丙氨酸2，（F5）苯丙氨酸4]-强啡肽1-13-NH2（DAFPHEDYN）：强啡肽1-13的一种强效类似物。

[D-Ala2, (F5) Phe4]-dynorphin 1-13-NH2 (DAFPHEDYN): a potent analog of dynorphin 1-13.

作者信息

Walker J M, Coy D H, Young E A, Baldrighi G, Siegel S F, Bowen W D, Akil H

机构信息

Department of Psychology, Brown University, Providence, RI 02912.

出版信息

Peptides. 1987 Sep-Oct;8(5):811-7. doi: 10.1016/0196-9781(87)90064-7.

DOI:10.1016/0196-9781(87)90064-7

PMID:2893357

Abstract

Intracerebroventricular administration of the dynorphin analog, [D-Ala2,(F5)Phe4]-dynorphin 1-13-NH2 (DAFPHEDYN) in rats produced diuresis and profound analgesia. Both effects were antagonized by central administration of naltrexone or naloxone. Intravenous administration of 10, 25, and 50 mg/kg of DAFPHEDYN failed to induce diuresis. The increased potency of DAFPHEDYN was apparent from the failure of an equal dose of the parent compound (dynorphin 1-13) to produce diuresis and the failure of [D-Ala2]-dynorphin 1-13-NH2 to produce analgesia. Radioligand binding studies indicated the DAFPHEDYN retains the same degree of kappa selectivity as the parent compound (dynorphin 1-13) though a drop in affinity occurred. DAFPHEDYN may be of significant interest because it retains the essential pharmacology of the parent compound and exhibits marked in vivo potency.

摘要

向大鼠脑室内注射强啡肽类似物[D - Ala2, (F5)Phe4]-强啡肽1 - 13 - NH2（DAFPHEDYN）可产生利尿和深度镇痛作用。这两种作用都可被中枢给予纳曲酮或纳洛酮所拮抗。静脉注射10、25和50mg/kg的DAFPHEDYN未能诱导利尿。从等剂量的母体化合物（强啡肽1 - 13）未能产生利尿以及[D - Ala2]-强啡肽1 - 13 - NH2未能产生镇痛作用可以明显看出DAFPHEDYN的效力增强。放射性配体结合研究表明，尽管亲和力有所下降，但DAFPHEDYN保留了与母体化合物（强啡肽1 - 13）相同程度的κ选择性。DAFPHEDYN可能具有重要意义，因为它保留了母体化合物的基本药理学特性并表现出显著的体内效力。